Products
Lopinavir is commercially available as film-coated tablets and as a syrup as a fixed combination with ritonavir (Kaletra). It has been approved in many countries since 2000.
Structure and properties
Lopinavir (C37H48N4O5, Mr = 628.8 g/mol) exists as a white to yellowish white powder that is practically insoluble in water.
Effects
Lopinavir (ATC J05AE06) has antiviral properties. The effects are due to inhibition of HIV protease, which plays a central role in viral maturation and replication. Lopinavir is combined fixed with the pharmacokinetic enhancer ritonavir. This is a CYP inhibitor that reduces metabolic degradation of the drug.
Indications
For the treatment of infections with HIV-1 (combination antiretroviral therapy). Off-label use:
- In 2020, lopinavir/ritonavir was used for infection with the new coronavirus (Covid-19). It is not approved for this use.
Dosage
According to the professional information. The drug is administered once or twice daily. The film-coated tablets can be taken with or independently of meals. The syrup should be taken with meals.
Contraindications
- Hypersensitivity
- Severe hepatic insufficiency
- Combination with certain drugs
Full precautions can be found in the drug label.
Interactions
Lopinavir is a substrate of CYP3A. Corresponding drug interactions with CYP substrates, inhibitors, and inducers are possible.
Adverse effects
The most common possible adverse effects include diarrhea, nausea, vomiting, abdominal pain, general weakness, headache, rash, sweating, abnormal stools, dyspepsia, flatulence, gastrointestinal disturbances, and insomnia.
